e-Drug3D

1454

FOSPROPOFOL

DISCONTINUED

INN
FOSPROPOFOL

(has an active metabolite)

cas 258516-89-1

CLASS

NERVOUS SYSTEM
SEDATIVE
HYPNOTIC
ANESTHESIC
METABOLIZED BY ALKALINE PHOSPHATASES INTO PROPOFOL

ROUTE (list)

INTRAVENOUS

ATC code

N01AX10

PK parameters

Cmax 732.6 MICROMOLAR (18 MILLIGRAM/KG)
VD 21.4 LITER (65 KILOGRAM)
Cl 18.2 LITER / HOUR (65 KILOGRAM)
PPB 98 PERCENT
t1/2 0.81 HOUR (18 MILLIGRAM/KG)

Solubility

WATER SOLUBLE PRODRUG OF PROPOFOL

Target

TARGET GAMMA-AMINOBUTYRIC-ACID RECEPTOR SUBUNIT ALPHA-1 (GABA(A))
BETA-ADRENOCEPTOR (BETA-AR) (PMID21793316)

PDB
8YRG (CRYOEM STRUCTURE OF FOSPROPOFOL-BOUND MRGPRX4-GQ COMPLEX)

Ligand code = A1LZU (link to the list of PDB complexes)

Download experimental 3D coordinates of A1LZU with added hydrogens

DrugCentral

GABA-A receptor alpha-1,beta-2,gamma-2 UNIPROT P14867 GABRA1

GABA-A receptor alpha-1,beta-3,gamma-2 UNIPROT P14867 GABRA1

Download SDF file

Methanol, 1-[2,6-bis(1-methylethyl)phenoxy]-, 1-(dihydrogen phosphate)

Formula:
C13H21O5P

Calculated chemical properties:

MW 286.25
NB_atoms 19
XLogP 2.11
PSA 71.38
NB_HD 0
NB_HA 5
fsp3 0.54
Lipinski(0=no;1=yes) 1

FDA
NDA 022244 (label) INN (FOSPROPOFOL DISODIUM) LUSEDRA (EISAI INC) APPROVAL= AP YEAR= 2008 NEWMOLECULARENTITY DISCONTINUED